建立了一锅法合成哌嗪酮取代醌类衍生物的方法.该方法以哌嗪酮烯胺酯为合成砌块,以乙腈为溶剂,醋酸作催化剂,在室温条件下,通过哌嗪酮烯胺酯1与醌类化合物2的α-C选择性烷基化反应,再经氧化脱氢简洁高效地合成了一系列结构新颖的哌嗪酮醌类衍生物3a-3l,产率70%-88%.该方法具有原料易得、合成路线简洁、产率高和操作简便等特点.
In this article, a one-pot protocol was established for the synthesis of ketopiperazine-substituted quinone derivatives. This method based on the building blocks of piperazine ketone enamine ester 1, which reacted with quinones 2 through α-C selective alkylation of the enamine ester and via dehydrogenation oxidation reaction in acetonitrile at room temperature and acetic acid as catalyst. As a result, a series of novel ketopiperzine-substituted quinone derivatives 3a-3l have been synthesized efficiently with 70%-88% yield. This method possesses some advantages such as simple synthetic route, readily available starting materials, high yields and simple work-up procedures.